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Bioorg Med Chem Lett. 2014 Dec 1;24(23):5357-63. doi: 10.1016/j.bmcl.2014.10.021. Epub 2014 Oct 13.

Antibody-drug conjugates—a new wave of cancer drugs.

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Natural Products and Protein Chemistry, Sanofi, 94403 Vitry-sur-Seine, France; Lead Generation to Compound Realization, Sanofi, 94403 Vitry-sur-Seine, France.
Lead Generation to Compound Realization, Sanofi, 94403 Vitry-sur-Seine, France. Electronic address:


Antibody-drug conjugates (ADCs) consist of cytotoxic drugs covalently linked to monoclonal antibodies directed to antigens differentially overexpressed in tumor cells. These loaded antibodies are expected to selectively deliver lethal cargoes to tumor cells and provide sustained clinical benefit to pre-selected cancer patients while, at the same time, minimizing systemic toxicity. Although on-target adverse events are not completely avoided and the true efficacy of these innovative agents still requires further clarification, proof-of-concept has already been achieved in clinical settings with immunoconjugates containing calicheamicin, auristatin or maytansine-based cytotoxic payloads. In this present article we review the characteristics of the preceding cytotoxic platforms and their chemical conjugation approaches.


Bioorganic; Conjugate; Linkers; Natural products; Oncology

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